Gliquidone References

Gliquidone
Clinical data
Trade names	Glurenorm
AHFS/ Drugs.com	International Drug Names
Pregnancy; category	C;
Routes of; administration	Oral ( tablets)
ATC code	A10BB08 ( WHO) ;
Legal status
Legal status	UK: POM (Prescription only); In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	High ( Tmax = 2–3 hours)
Metabolism	Extensive hepatic
Onset of action	1–1.5 hours
Excretion	Biliary (95%), renal (5%)
Identifiers
	IUPAC name 1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]phenyl]sulfonylurea;
CAS Number	33342-05-1;
PubChem CID	91610;
DrugBank	DB01251 ;
ChemSpider	82719 ;
UNII	C7C2QDD75P;
KEGG	D02430 ;
ChEMBL	ChEMBL383634 ;
CompTox Dashboard ( EPA)	DTXSID4023096 ;
ECHA InfoCard	100.046.770
Chemical and physical data
Formula	C27H33N3O6S
Molar mass	527.64 g·mol−1
3D model ( JSmol)	Interactive image;
	SMILES O=C(NC1CCCCC1)NS(=O)(=O)c2ccc(cc2)CCN4C(=O)c3c(ccc(OC)c3)C(C4=O)(C)C;
	InChI InChI=1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33) ; Key:LLJFMFZYVVLQKT-UHFFFAOYSA-N ;
	(verify)

Gliquidone ( INN, sold under the trade name Glurenorm) is an anti-diabetic medication in the sulfonylurea class.^[1] It is classified as a second-generation sulfonylurea. It is used in the treatment of diabetes mellitus type 2. It is marketed by the pharmaceutical company Boehringer Ingelheim (Germany).

Contraindications

Allergy to sulfonylureas or sulfonamides
Diabetes mellitus type 1
Diabetic ketoacidosis
Patients that underwent removal of the pancreas
Acute porphyria
Severe liver disease accompanying with liver insufficiency
Several conditions (e.g., infectious diseases or major surgical intervention), when insulin administration is required
Pregnancy or breastfeeding^[2]

Pharmacokinetics

Gliquidone is fully metabolized by the liver. Its metabolites are excreted virtually completely with bile (even with long-term administration), thus allowing the use of medication in diabetic patients with kidney disease and diabetic nephropathy.^[2]

References

^ Malaisse WJ (2006). "Gliquidone contributes to improvement of type 2 diabetes mellitus management: a review of pharmacokinetic and clinical trial data". Drugs in R&D. 7 (6): 331–7. doi: 10.2165/00126839-200607060-00002. PMID 17073516. S2CID 10155445.
^ ^a ^b "Glurenorm (gliquidone) 30 mg Tablets, for Oral Use. Full Prescribing Information". Russian State Register of Medicinal Products (in Russian). Boehringer Ingelheim. Archived from the original on 14 August 2016. Retrieved 12 July 2016.

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[Malaisse_2006-1] Malaisse WJ (2006). "Gliquidone contributes to improvement of type 2 diabetes mellitus management: a review of pharmacokinetic and clinical trial data". Drugs in R&D. 7 (6): 331–7. doi: 10.2165/00126839-200607060-00002. PMID 17073516. S2CID 10155445.

[PI-2] "Glurenorm (gliquidone) 30 mg Tablets, for Oral Use. Full Prescribing Information". Russian State Register of Medicinal Products (in Russian). Boehringer Ingelheim. Archived from the original on 14 August 2016. Retrieved 12 July 2016.

[1]

[2]

Clinical data

Trade names	Glurenorm
AHFS/ Drugs.com	International Drug Names
Pregnancy category	C
Routes of administration	Oral ( tablets)
ATC code	A10BB08 ( WHO)
Legal status
Legal status	UK: POM (Prescription only) In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	High ( T_max = 2–3 hours)
Metabolism	Extensive hepatic
Onset of action	1–1.5 hours
Excretion	Biliary (95%), renal (5%)
Identifiers
IUPAC name 1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]phenyl]sulfonylurea
CAS Number	33342-05-1
PubChem CID	91610
DrugBank	DB01251^Y
ChemSpider	82719^Y
UNII	C7C2QDD75P
KEGG	D02430^Y
ChEMBL	ChEMBL383634^Y
CompTox Dashboard ( EPA)	DTXSID4023096
ECHA InfoCard	100.046.770
Chemical and physical data
Formula	C₂₇H₃₃N₃O₆S
Molar mass	527.64 g·mol⁻¹
3D model ( JSmol)	Interactive image
SMILES O=C(NC1CCCCC1)NS(=O)(=O)c2ccc(cc2)CCN4C(=O)c3c(ccc(OC)c3)C(C4=O)(C)C
InChI InChI=1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33)^Y Key:LLJFMFZYVVLQKT-UHFFFAOYSA-N^Y
(verify)